Benzodiazapines have been used as therapeutics. Benzodiazepine derivatives include pyrrolobenzodiazepines. Pyrrolobenzodiazepine dimers function as DNA cross-linking agents, e.g., by binding in the minor groove of DNA molecules. Certain of these have been suggested as antiproliferative agents in the treatment of cancer.
Duocarmycins also have been used as therapeutics. Duocarmycins bind to the minor groove of DNA. They alkylate the adenine at the N3 position. The general structure of Duocarmycin has two key components—a DNA alkylation unit, such as 1-(chloromethyl)-2,3-dihydro-1H-benzo[e]indole (CBI), and an indole-2 carbonyl unit that non-covalently binds DNA.